天然活性先导化合物生物转化研究进展

天然活性先导化合物生物转化是利用生物催化剂(如：酶、微生物、动植物细胞)将加入到生物反应系统中的天然活性先导化合物进行特异性的分子结构修饰以获得高效、低毒新化合物的方法。该方法可以有效地提高已知的天然活性先导化合物的活性、降低毒副作用、改善水溶性和生物利用度，也可以用来生产具有重要应用价值的微量天然活性先导化合物，同时可用于药物代谢机制的研究。国内外学者已经针对甾体、醌类、黄酮类、萜类等化合物开展了天然活性先导化合物生物转化研究，筛选出一批有重要应用价值的生物转化反应类型，但针对天然活性先导化合物生物转化的机制、生物转化过程工程以及生物转化产物活性等方面的研究较少。将现代生命科学技术(如：生物催化剂的定向改造、高通量筛选、组合生物转化、非水相生物转化)引入天然活性先导化合物生物转化研究中，必将推进天然活性先导化合物的快速发展。

Advance on the Biotransformation of Bioactive Natural Leading Compounds

Biotransformation of bioactive natural leading compounds is a kind of bioprocess in which the structure of the added bioactive natural leading compounds could be modified by biocatalysts(e.g.,enzyme,microbial,plant and animal cells) in order to produce high efficient and low toxicity compounds.The biotransformation purpose of the known bioactive natural leading compounds is to improve its efficiency,or reduce its toxicity,or improve its solubility and bioavailability.The trace and high-valued bioactive natural leading compounds also could be produced by the biotransformation,and the biotransformation of bioactive natural leading compounds is still helpful to study the mechanism of drug metabolism.The current focus of the biotransformation of bioactive natural leading compounds is on the compounds of steroid,quinine,flavone and terpene,and some important biotransformation process has been successfully screened out.Fundamental research should be done in the following fields,such as the biotransformation mechanism of bioactive natural leading compounds,biotransformation process engineering,and the efficiency evaluation of bioproducts produced by biotransformation.The latest biotechnology(e.g.,directed evolution of biocatalyst,combinatorial biotransformation,non-aqueous biotransformation,high throughput screening) should be introduced to the biotransformation of bioactive natural leading compounds,which will boost its fast development.